As to effectiveness of heterocyclic amine derivatives (e.g. isocoumarin, isoquinolone, benzothiopyran, etc.) for the therapy of arteriosclerosis or for lowering cholesterol in blood, no sufficient study has been conducted.
The present invention principally provides novel heterocyclic amine derivatives having an excellent activity of inhibiting acyl-CoA:cholesterol acyltransferase, controlling, in mammals, absorption of cholesterol from the intestinal tract and suppressing accumulation of cholesterol ester at the arterial wall, thus being useful for the prophylaxis and therapy of hypercholesterolemia, atherosclerosis and various diseases caused by them (e.g. ischemic heart diseases such as cardiac infarction and cerebral blood vessel disorders such as cerebral infarction, apoplexy, etc.). The present invention further provides an industrially advantageous method of producing these novel compounds and also compositions or agents useful as medicines containing these novel compounds.